Structural study of phenyl boronic acid derivatives as AmpC β-lactamase inhibitors

D Tondi, S Calò, BK Shoichet, MP Costi

Index: Tondi, Donatella; Calo, Samuele; Shoichet, Brian K.; Costi, Maria Paola Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 11 p. 3416 - 3419

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Citation Number: 24

Abstract

A small set of boronic acids acting as low nanomolar inhibitors of AmpC β-lactamase were designed and synthesized in the effort to improve affinity, pharmacokinetic properties, and to provide a valid lead compound. X-ray crystallography revealed the binary complex of the best inhibitor bound to the enzyme, highlighting possibilities for its further rational derivatization and chemical optimization.